WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205743
Description: Serabelisib (also known as MLN1117, INK1117, and TAK-117) is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity. PI3K alpha inhibitor INK1117 selectively inhibits PI3K alpha kinase, including mutations of PIK3CA, in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K alpha-expressing tumor cells. By specifically targeting class I PI3K alpha, this agent may be more efficacious and less toxic than pan-PI3K inhibitors.
MedKoo Cat#: 205743
Chemical Formula: C19H17N5O3
Exact Mass: 363.1331
Molecular Weight: 363.377
Elemental Analysis: C, 62.80; H, 4.72; N, 19.27; O, 13.21
Synonym: INK1117; INK-1117; INK 1117; MLN1117; MLN 1117; MLN-1117; TAK-117; TAK 117; TAK117; Serabelisib
IUPAC/Chemical Name: [6-(2-amino-5-benzoxazolyl)imidazo[1,2-a]pyridin-3-yl]-4-morpholinyl-methanone
InChi Key: BLGWHBSBBJNKJO-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H17N5O3/c20-19-22-14-9-12(1-3-16(14)27-19)13-2-4-17-21-10-15(24(17)11-13)18(25)23-5-7-26-8-6-23/h1-4,9-11H,5-8H2,(H2,20,22)
SMILES Code: O=C(C1=CN=C2C=CC(C3=CC=C(OC(N)=N4)C4=C3)=CN21)N5CCOCC5
INK1117 has demonstrated significant efficacy in several PI3Kα mutant-specific preclinical mouse xenograft tumor models. Moreover, daily oral administration of INK1117 inhibited tumor growth in a dose-dependent manner with a predicted PK/PD relationship, was well tolerated at a range of efficacious doses, and exhibited several differentiating features from less selective inhibitors that target the PI3K/Akt/mTOR pathway. A Phase I dose escalation study is underway to evaluate the safety, tolerability and pharmacokinetics of single-agent INK1117 in patients with advanced solid malignancies who have tumors characterized by the presence of a PIK3CA mutation. (source: http://www.intellikine.com/pipeline/pi3kalpha_inhibitors.html).
1: Yea SS, So L, Mallya S, Lee J, Rajasekaran K, Malarkannan S, Fruman DA.
Effects of novel isoform-selective phosphoinositide 3-kinase inhibitors on
natural killer cell function. PLoS One. 2014 Jun 10;9(6):e99486. doi:
10.1371/journal.pone.0099486. eCollection 2014. PubMed PMID: 24915189; PubMed
Central PMCID: PMC4051752.
2: So L, Yea SS, Oak JS, Lu M, Manmadhan A, Ke QH, Janes MR, Kessler LV,
Kucharski JM, Li LS, Martin MB, Ren P, Jessen KA, Liu Y, Rommel C, Fruman DA.
Selective inhibition of phosphoinositide 3-kinase p110α preserves lymphocyte
function. J Biol Chem. 2013 Feb 22;288(8):5718-31. doi: 10.1074/jbc.M112.379446.
Epub 2012 Dec 28. PubMed PMID: 23275335; PubMed Central PMCID: PMC3581375.